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Overview
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Background
Oleoyl Ethyl Amide (OEtA) is a potent fatty amide acyl hydrolase (FAAH) inhibitor with potential analgesic and anxiolytic activity [1]. Fatty acid amide hydrolase (FAAH) is an integral membrane hydrolase and a member of the serine hydrolase family of enzymes. In vitro, FAAH has esterase and amidase activity. In vivo, FAAH is the principal catabolic enzyme for the fatty acid amides (FAAs). Oleoyl Ethyl Amide (OEtA) is a potent fatty amide acyl hydrolase (FAAH) inhibitor. In rat brain homogenates, Oleoyl Ethyl Amide inhibited FAAH activity with IC50 value of 5.25 nM, but did not bind to CB1 or CB2 receptors, or inhibit acidic PEAase. Oleoyl Ethyl Amide is a potent and selective FAAH inhibitor with potential analgesic and anxiolytic activity [1]. In Sprague-Dawley rats, subcutaneous injections of OEtA (0.3 mg/kg) for 2 weeks increased values of micturition intervals (MI) and volumes (MV), bladder capacity (BC), threshold pressure, and flow pressure. OEtA altered sensory urodynamic parameters and reduced bladder overactivity [2].
[1]. Vandevoorde, S.,Lavand'homme, P.,Fowler, C.J., et al. Oleoylethylamide, an analgesic FAAH inhibitor which modulates endogenous anandamide, oleoylethanolamide, and 2-arachidonoylglycerol levels in the brain. 14th Annual Symposium on the Cannabinoids 15-15 (2004).
[2]. Gandaglia G, Strittmatter F, La Croce G, et al. The fatty acid amide hydrolase inhibitor oleoyl ethyl amide counteracts bladder overactivity in female rats. Neurourol Urodyn. 2014 Nov;33(8):1251-8.
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